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thiamphenicol

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Thiamphenicol is a synthetic broad-spectrum antibiotic that is chemically related to chloramphenicol. It is effective against a wide range of gram-positive and gram-negative bacteria. Thiamphenicol is synthesized by a multi-step process starting with the reaction of p-nitrobenzaldehyde with nitroethane to form 2-nitro-1-(p-nitrophenyl)propane. This compound is then reduced to the corresponding amine and then reacted with chloroacetyl chloride to give thiamphenicol. Thiamphenicol inhibits protein synthesis in bacteria by binding to the 50S subunit of the bacterial ribosome, preventing the formation of peptide bonds. It has been used to treat a variety of infections, including pneumonia, meningitis, and typhoid fever. However, it has been associated with serious side effects, including aplastic anemia, and its use is therefore restricted in many countries. Research into thiamphenicol has been largely focused on its mechanism of action and its potential as a therapeutic agent. However, the development of newer antibiotics with a wider spectrum of activity and fewer side effects has led to a decrease in the use of thiamphenicol in clinical practice.'

Cross-References

ID SourceID
PubMed CID27200
CHEMBL ID1236282
CHEBI ID32215
SCHEMBL ID34635
MeSH IDM0021328

Synonyms (161)

Synonym
2,2-dichloro-n-{(1r,2r)-2-hydroxy-1-(hydroxymethyl)-2-[4-(methylsulfonyl)phenyl]ethyl}acetamide
(+)-thiamphenicol
CHEBI:32215 ,
d-(+)-threo-2,2-dichloro-n-(beta-hydroxy-alpha-(hydroxymethyl)-p-(methylsulfonyl)phenethyl)acetamide
thiamphenicol dl-form
win-5063
acetamide, 2,2-dichloro-n-(beta-hydroxy-alpha-(hydroxymethyl)-p-(methylsulfonyl)phenethyl)-, threo-(+-)-
racefenicol [inn]
racephenicol [usan]
(+-)-threo-2,2-dichloro-n-(beta-hydroxy-alpha-(hydroxymethyl)-p-(methylsulfonyl)phenethyl)acetamide
dl-threo-2-dichloroacetamido-1-(4-methylsulfonyl-phenyl)-1,3-propanediol
unii-283383no13
acetamide, 2,2-dichloro-n-(2-hydroxy-1-(hydroxymethyl)-2-(4-(methylsulfonyl)phenyl)ethyl)-, (r*,r*)-(+-)-
283383no13 ,
acetamide, 2,2-dichloro-n-((1r,2r)-2-hydroxy-1-(hydroxymethyl)-2-(4-(methylsulfonyl)phenyl)ethyl)-, rel-
racefenicolo
racefenicolum
racefenicolo [dcit]
thiamphenicol dl-
racefenicolum [inn-latin]
th8 ,
MLS002154177
BRD-K79711234-001-06-8
CHEMBL1236282
armai
8065 c.b.
DIVK1C_000842
KBIO1_000842
acetamide, 2,2-dichloro-n-(2-hydroxy-1-(hydroxymethyl)-2-(4-(methylsulfonyl)phenyl)ethyl)-, (r-(r*,r*))-
acetamide, 2,2-dichloro-n-(beta-hydroxy-alpha-(hydroxymethyl)-p-(methylsulfonyl)phenethyl)-, d-threo-(+)
d-thiocymetin
thiamphenicolum [inn-latin]
acetamide, 2,2-dichloro-n-((1r,2r)-2-hydroxy-1-(hydroxymethyl)-2-(4-(methylsulfonyl)phenyl)ethyl)-
win-5063-2
d-threo-(1r,2r)-1-(p-methylsulfonylphenyl)-2-dichloroacetamido-1,3-propanediol
tiamfenicol [inn-spanish]
d-d-threo-2-dichloroacetamido-1-(4-methylsulfonylphenyl)-1,3-propanediol
thiamphenicol [usan:inn:ban:jan]
d-thiophenicol
raceophenidol
einecs 239-355-3
nsc 522822
tiamfenicolo [dcit]
SPECTRUM_001428
SPECTRUM5_001617
PRESTWICK_885
SMP2_000125
IDI1_000842
NCGC00178319-01
NCGC00178319-02
thiamphenicol ,
15318-45-3
PRESTWICK3_000025
BPBIO1_000099
PRESTWICK2_000025
smr000857096
MLS001332639
MLS001332640 ,
win 5063-2
igralin
urfamycine
dexawin
thiocymetin
nsc-522822
dextrosulphenidol
thiophenicol
thiocymetin (tn)
D01407
armai (tn)
thiamphenicol (jan/usan/inn)
BSPBIO_000089
BSPBIO_003064
KBIO2_001908
KBIO2_004476
KBIO2_007044
KBIOSS_001908
KBIOGR_001026
KBIO3_002564
SPECTRUM2_000856
SPECTRUM4_000733
SPECTRUM3_001562
PRESTWICK1_000025
SPBIO_000871
PRESTWICK0_000025
SPBIO_002010
NINDS_000842
SPECTRUM1503136
HMS2092L18
DB08621
HMS502K04
HMS1922G19
HMS1568E11
2,2-dichloro-n-[(1r,2r)-1,3-dihydroxy-1-(4-methylsulfonylphenyl)propan-2-yl]acetamide
A809401
2,2-dichloro-n-((1r,2r)-1,3-dihydroxy-1-(4-(methylsulfonyl)phenyl)propan-2-yl)acetamide
NCGC00178319-03
HMS2095E11
T2802
2,2-dichloro-n-[(1r,2r)-1,3-dihydroxy-1-[4-(methylsulfonyl)phenyl]-2-propyl]acetamide
unii-flq7571npm
tiamfenicol
tiamfenicolo
ccris 8588
flq7571npm ,
NCGC00258370-01
tox21_200816
nsc-758396
pharmakon1600-01503136
nsc758396
tox21_110577
dtxcid801338
dtxsid5021338 ,
thiamphenicolum
AKOS015951269
HMS2232E21
CCG-40309
NCGC00178319-07
thiamphenicol [mart.]
thiamphenicol [mi]
thiamphenicol [ep monograph]
thiamphenicol [jan]
thiamphenicol [inn]
2,2-dichloro-n-((1r,2r)-2-hydroxy-1-(hydroxymethyl)-2-(4-(methylsulfonyl)phenyl)ethyl)acetamide
thiamphenicol [usan]
thiamphenicol [who-dd]
S2583
HY-B0479
SCHEMBL34635
NCGC00178319-06
tox21_110577_1
acetamide, 2,2-dichloro-n-(2-hydroxy-1-(hydroxymethyl)-2-(4-(methylsulfonyl)phenyl)ethyl)-, (r*,r*)-(+/-)-
acetamide, 2,2-dichloro-n-(.beta.-hydroxy-.alpha.-(hydroxymethyl)-p-(methylsulfonyl)phenethyl)-, threo-(+/-)-
thiamphenicol dl-form [mi]
(+/-)-thiamphenicol
OTVAEFIXJLOWRX-NXEZZACHSA-N
2,2-bis(chloranyl)-n-[(1r,2r)-1-(4-methylsulfonylphenyl)-1,3-bis(oxidanyl)propan-2-yl]ethanamide
bdbm58925
cid_27200
2,2-dichloro-n-[(1r,2r)-2-hydroxy-2-(4-mesylphenyl)-1-methylol-ethyl]acetamide
AB00052321_11
AB00052321_10
mfcd00467983
sr-05000001829
SR-05000001829-3
thiamphenicol, analytical standard
SR-05000001829-1
thiamphenicol, european pharmacopoeia (ep) reference standard
SBI-0051779.P002
HMS3712E11
2,2-dichloro-n-[(1r,2r)-1,3-dihydroxy-1-(4-methanesulfonylphenyl)propan-2-yl]acetamide
SW197006-3
Q425015
thiamphenicol (thiophenicol)
thiophenicol;dextrosulphenidol
AS-12501
BRD-K79711234-001-11-8
BCP32746
thiophenicol; dextrosulphenidol; descocin; hyrazin; masatirin; urfamycine
acetamide,2,2-dichloro-n-[(1r,2r)-2-hydroxy-1-(hydroxymethyl)-2-[4-(methylsulfonyl)phenyl]ethyl]-
gtpl12400
thiamphenicol 1000 microg/ml in acetonitrile

Research Excerpts

Overview

Thiamphenicol (TAP) is an amphenicol antibiotic, which has a broad-spectrum inhibitory effect on both gram-positive and gram-negative bacteria. It is a typical medicament in animal husbandry and aquaculture for treating diverse infections.

ExcerptReferenceRelevance
"Thiamphenicol (TAP) is an amphenicol antibiotic, which has a broad-spectrum inhibitory effect on both gram-positive and gram-negative bacteria. "( Removal of antibiotic thiamphenicol by bacterium Aeromonas hydrophila HS01.
Ai, Z; Jin, Y; Mei, M; Ren, S; Shi, Z; Xiang, W; Xie, B; Yang, K; Yi, L, 2022
)
2.48
"Thiamphenicol (TAP) is a typical medicament in animal husbandry and aquaculture for treating diverse infections. "( Biodegradation and metabolic fate of thiamphenicol via Chlorella sp. UTEX1602 and L38.
Kitamura, Y; Li, S; Song, C; Song, Y; Sun, J; Wei, Y, 2020
)
2.27
"Thiamphenicol is an antimicrobial agent active in the treatment of infection of different etiology and localisation due to its broad spectrum of antimicrobial activity as well as its pharmacokinetic properties."( Aerosol therapy with thiamphenicol glycinate: a retrospective study on efficacy and safety in a group of sixty-six oncological patients.
Castelnuovo, P; Macchi, A; Macchi, S; Roselli, R; Terranova, P,
)
1.17
"Thiamphenicol is a broad-spectrum antimicrobial agent active against penicillin-resistant Streptococcus pneumoniae, Staphylococcus aureus VISA strains, most methicillin-resistant isolates and atypical pathogens such as Mycoplasma pneumoniae and Chlamydia pneumoniae). "( Recent clinical evidence of the efficacy and safety of thiamphenicol glycinate acetylcysteinate and thiamphenicol glycinate.
De Benedetto, F; Grassi, C, 2002
)
2
"Thiamphenicol is a derivative of chloramphenicol characterized by a spectrum comparable to that of the parent compound against multiresistant pathogens but showing satisfactory tolerability. "( In vitro activity of thiamphenicol against multiresistant Streptococcus pneumoniae, Haemophilus influenzae and Staphylococcus aureus in Italy.
Debbia, EA; Gualco, L; Marchese, A; Schito, AM; Tonoli, E, 2002
)
2.08
"Thiamphenicol is an analogue of chloramphenicol and is characterised by a broad spectrum of action. "( Serum and lung levels of thiamphenicol after administration of its glycinate N-acetylcysteinate ester in experimentally infected guinea pigs.
De Vecchi, E; Drago, L; Fassina, MC; Gismondo, MR; Mombelli, B, 2000
)
2.05

Effects

ExcerptReferenceRelevance
"Thiamphenicol (1 g/kg) has no effect under the same conditions."( [Effects of chloramphenicol and thiamphenicol on sleep of the mouse].
Kitahama, K; Valatx, JL, 1975
)
1.26

Actions

ExcerptReferenceRelevance
"Thiamphenicol is known to produce two hematological side effects: a decrease in blood cell count concerning mainly red blood cells; in this case regression is observed after withdrawal of the drug; the frequency of this side effect appears to be higher than that observed after chloramphenicol administration. "( [Hematotoxicity of thiamphenicol. Report of two cases of acute erythroblastopenia (author's transl)].
Baufle, GH; Broda, C; Estavoyer, JM; Singer, P,
)
1.9

Treatment

Thiamphenicol-pretreated cells were bathed in anti-VIIa-L oligonucleotides. The recovery rate of COX activity compared to control oligomer-untreated cells or cells with a similar concentration of a randomized oligomer.

ExcerptReferenceRelevance
"Thiamphenicol-pretreated cells were bathed in anti-VIIa-L oligonucleotides and the recovery rate of COX activity compared to control oligomer-untreated cells or cells with a similar concentration of a randomized oligomer."( An antisense oligodeoxynucleotide approach to investigate the function of the nuclear-encoded subunits of human cytochrome c oxidase.
Bindoff, LA; Chrzanowska-Lightowlers, ZM; Lightowlers, RN; Turnbull, DM, 1993
)
1.01
"Treatment of thiamphenicol with hexamethyldisilazane or N-trimethylsilylimidazole, either alone or in the presence of trimethylchlorosilane, in acetonitrile or pyridine yields the bis(trimethylsily) (TMS) ether derivative."( Preparation of trimethylsilyl derivatives of thiamphenicol.
Janssen, G; Vanderhaeghe, H, 1977
)
0.87

Toxicity

ExcerptReferenceRelevance
"Thiamphenicol is known to produce two hematological side effects: a decrease in blood cell count concerning mainly red blood cells; in this case regression is observed after withdrawal of the drug; the frequency of this side effect appears to be higher than that observed after chloramphenicol administration."( [Hematotoxicity of thiamphenicol. Report of two cases of acute erythroblastopenia (author's transl)].
Baufle, GH; Broda, C; Estavoyer, JM; Singer, P,
)
1.9
" Both treatments were well tolerated with fewer than 5% of patients experiencing an adverse event."( Recent clinical evidence of the efficacy and safety of thiamphenicol glycinate acetylcysteinate and thiamphenicol glycinate.
De Benedetto, F; Grassi, C, 2002
)
0.56
" It was found that OXT and FLO have a stronger adverse effect on duckweed (EC50=3."( Aquatic toxicity of four veterinary drugs commonly applied in fish farming and animal husbandry.
Białk-Bielińska, A; Kołodziejska, M; Kumirska, J; Maszkowska, J; Stepnowski, P; Steudte, S; Stolte, S, 2013
)
0.39
"A simple and simultaneous method for the determination of florfenicol and its metabolite florfenicol amine in agricultural soils using modified quick, easy, cheap, effective, rugged, and safe sample pretreatment and reversed-phase high-performance liquid chromatography with tandem mass spectrometry is presented."( Simultaneous determination of florfenicol with its metabolite based on modified quick, easy, cheap, effective, rugged, and safe sample pretreatment and evaluation of their degradation behavior in agricultural soils.
Ma, J; Qian, M; Wang, J; Wu, H; Xu, M; Zhang, H, 2015
)
0.42
"Although modes of action (MOAs) play a key role in the understanding of the toxic mechanism of chemicals, the MOAs have not been investigated for antibiotics to green algae."( Toxicity of 13 different antibiotics towards freshwater green algae Pseudokirchneriella subcapitata and their modes of action.
Fu, L; Huang, T; Li, C; Su, L; Wang, S; Wang, X; Zhao, Y, 2017
)
0.46
" Adverse events were similar between groups."( A randomized placebo-controlled trial of the efficacy and safety of a terbinafine, florfenicol and betamethasone topical ear formulation in dogs for the treatment of bacterial and/or fungal otitis externa.
Doucette, KP; Forster, SL; King, SB; Real, T, 2018
)
0.48
"The application of two doses of Osurnia, one week apart, is effective and safe to treat microbial otitis externa in dogs."( A randomized placebo-controlled trial of the efficacy and safety of a terbinafine, florfenicol and betamethasone topical ear formulation in dogs for the treatment of bacterial and/or fungal otitis externa.
Doucette, KP; Forster, SL; King, SB; Real, T, 2018
)
0.48
" Adverse events attributable to the ear medications were not noted."( A randomized, controlled, single-blinded, multicenter evaluation of the efficacy and safety of a once weekly two dose otic gel containing florfenicol, terbinafine and betamethasone administered for the treatment of canine otitis externa.
Doucette, KP; Forster, SL; King, SB; Seewald, W, 2018
)
0.48
"Administering an otic gel twice at a one-week interval is an effective, safe and convenient way to treat canine otitis externa."( A randomized, controlled, single-blinded, multicenter evaluation of the efficacy and safety of a once weekly two dose otic gel containing florfenicol, terbinafine and betamethasone administered for the treatment of canine otitis externa.
Doucette, KP; Forster, SL; King, SB; Seewald, W, 2018
)
0.48
" This study suggests that the toxic effects of contaminants and NNPs on aquatic organisms should be considered thoroughly to avoid underestimating the hazard of these pollutants in the actual aquatic environment."( Effects of natural nanoparticles on the acute toxicity, chronic effect, and oxidative stress response of phenicol antibiotics in Daphnia magna.
Deng, J; Guo, P; Su, H; Sun, Y; Wang, M; Wu, Y; Zhang, Y, 2023
)
0.91

Pharmacokinetics

Study evaluated the pharmacokinetic disposition of thiamphenicol (THA) and florfenicol (FLR) after oral administration of each at a single dose of 10 mg/kg body weight in Pacific white shrimp.

ExcerptReferenceRelevance
"The pharmacokinetic disposition of florfenicol was studied in male veal calves given 11 mg of florfenicol/kg of body weight, IV and 11 mg of florfenicol/kg PO every 12 hours for 7 doses."( Tissue concentrations and pharmacokinetics of florfenicol in male veal calves given repeated doses.
Adams, PE; Lamendola, JF; Powers, TE; Varma, KJ, 1987
)
0.27
"The pharmacokinetic disposition of florfenicol was described in veal calves after administration of a single 22-mg/kg dose intravenously, orally after a 12-h fast and orally 5 min post feeding."( Pharmacokinetics of florfenicol in veal calves.
Adams, PE; Lamendola, JF; Powers, JD; Powers, TE; Varma, KJ, 1986
)
0.27
" The terminal half-life after intravenous administration was 159 min."( Pharmacokinetics of florfenicol following intravenous and intramuscular doses to cattle.
Ashcraft, SM; Gerken, DF; Johnson, JC; Lobell, RD; Sams, RA; Varma, KJ, 1994
)
0.29
" The rate at which thiamphenicol appeared in the milk, as indicated by the penetration half-life (t1/2P) (serum to quarters), was found to be 36."( The pharmacokinetics of thiamphenicol in lactating cows.
Alt, M; Errecalde, JO; Landoni, MF; Mestorino, N, 1993
)
0.92
" injection, the kinetic disposition of florfenicol followed a two-compartmental open model with an elimination half-life of 172 min, total body clearance of 26."( Tissue concentrations and pharmacokinetics of florfenicol in broiler chickens.
Afifi, NA; EL-SOOUD, KA, 1997
)
0.3
" injection, the kinetic disposition of florfenicol followed a 2-compartmental open model with an elimination half-life of 173 min, total body clearance of 26."( Tissue concentrations and pharmacokinetics of florfenicol in broiler chickens.
Abo el-Sooud, KA; Afifi, NA, 1997
)
0.3
" The maximum serum concentration of florfenicol in control healthy and infected ducks was reached 1 hour after intramuscular injection but the peak concentration in control ducks was higher than in infected birds."( Pharmacokinetics of florfenicol in normal and Pasteurella-infected Muscovy ducks.
el-Banna, HA, 1998
)
0.3
"To determine pharmacokinetic parameters of thiamphenicol (TAP) after IV and IM administration in dogs."( Pharmacokinetics of thiamphenicol in dogs.
Arboix, M; Castells, G; Cristòfol, C; Franquelo, C; Intorre, L; Martí, G; Pérez, B, 1998
)
0.89
" Elimination half-life was short (1."( Pharmacokinetics of thiamphenicol in dogs.
Arboix, M; Castells, G; Cristòfol, C; Franquelo, C; Intorre, L; Martí, G; Pérez, B, 1998
)
0.62
"The pharmacokinetic profile of TAP in dogs suggests that it may be therapeutically useful against susceptible microorganisms involved in the most common infections in dogs, such as tracheobronchitis, enterocolitis, mastitis, and urinary tract infections."( Pharmacokinetics of thiamphenicol in dogs.
Arboix, M; Castells, G; Cristòfol, C; Franquelo, C; Intorre, L; Martí, G; Pérez, B, 1998
)
0.62
"Although the in vitro activity of the tested drugs evaluated by time-kill curves seemed comparable, some pharmacokinetic and pharmacodynamic characteristics of TGA contribute to improving the resolution of the infective process."( Comparative effect of thiamphenicol glycinate, thiamphenicol glycinate N-acetylcysteinate, amoxicillin plus clavulanic acid, ceftriaxone and clarithromycin on pulmonary clearance of Haemophilus influenzae in an animal model.
De Vecchi, E; Drago, L; Fassina, MC; Gismondo, MR; Lombardi, A; Mombelli, B,
)
0.45
" In diseased broiler chickens, a decrease in the elimination half-life and the apparent volume of distribution were found."( Pharmacokinetics of florfenicol in healthy and Escherichia coli-infected broiler chickens.
Hu, D; Jiang, H; Shen, J; Wu, X, 2002
)
0.31
"A comparative in vivo pharmacokinetic study of florfenicol was conducted in 18 crossbred pigs infected with Actinobacillus pleuropneumoniae following intravenous (i."( Pharmacokinetics of florfenicol in healthy pigs and in pigs experimentally infected with Actinobacillus pleuropneumoniae.
Chen, Z; Fung, KF; Liu, J; Zeng, Z; Zhang, J, 2003
)
0.32
"The aim of this study has been to determine the tissue pharmacokinetic parameters of florfenicol in the pigs experimentally infected with Actinobacillus pleuropneumoniae."( Tissue pharmacokinetics of florfenicol in pigs experimentally infected with Actinobacillus pleuropneumoniae.
Chen, ZL; Fung, KF; Li, JZ; Zeng, ZL; Zhang, J,
)
0.13
"Tissue pharmacokinetic data could be evidence for regime designing of florfenicol in treatment of porcine pleuropneumonia."( Tissue pharmacokinetics of florfenicol in pigs experimentally infected with Actinobacillus pleuropneumoniae.
Chen, ZL; Fung, KF; Li, JZ; Zeng, ZL; Zhang, J,
)
0.13
" Pharmacokinetic analysis was performed using a two-compartment open model."( Comparative plasma pharmacokinetics and tolerance of florfenicol following intramuscular and intravenous administration to camels, sheep and goats.
Al-Qarawi, AA; Ali, BH; Hashaad, M, 2003
)
0.32
"The pharmacokinetic profile of the antibacterial agent florfenicol was studied in plasma after intravenous (i."( Pharmacokinetics of florfenicol in cod Gadus morhua and in vitro antibacterial activity against Vibrio anguillarum.
Bergh, O; Ervik, A; Samuelsen, OB, 2003
)
0.32
"The bioavailability and pharmacokinetic disposition of florfenicol in broiler chickens were investigated after intravenous (i."( Bioavailability and pharmacokinetics of florfenicol in broiler chickens.
Coats, JR; Hu, D; Shen, J; Wu, X, 2003
)
0.32
" The concentration of florfenicol in serum samples was assayed using a proprietary HPLC assay method, and pharmacokinetic parameters derived for individual animal data by each route using compartmental and noncompartmental approaches."( Intravenous and subcutaneous pharmacokinetics of florfenicol in sheep.
Clifford, A; Craigmill, AL; Lane, VM; Taylor, I; Villarroel, A; Wetzlich, S; Wetzlich, SE, 2004
)
0.32
" Florfenicol pharmacokinetic parameters in elk were estimated using a noncompartmental approach."( Pharmacokinetics of florfenicol in North American elk (Cervus elaphus).
Alcorn, J; Dowling, P; Killeen, R; Woodbury, M, 2004
)
0.32
" florfenicol injection (as a bolus), the terminal half-life (t(1/2)), the volume of distribution at steady state (V(dss)), and total body clearance were 11."( Pharmacokinetics of florfenicol and its metabolite, florfenicol amine, in the Korean catfish (Silurus asotus).
Kim, MS; Lim, JH; Park, BK; Yun, HI, 2006
)
0.33
" Application of this method demonstrated that it was feasible for the clinical pharmacokinetic study."( Simultaneous analysis of thiamphenicol and its prodrug thiamphenicol glycinate in human plasma and urine by high performance liquid chromatography: application to pharmacokinetic study.
Chen, X; Ni, L; Wang, G; Yang, B, 2006
)
0.64
" Pharmacokinetic variables of the drug were calculated after both administration routes."( Capillary electrophoretic determination of thiamphenicol in turkeys serum and its pharmacokinetic application.
Kowalski, P, 2007
)
0.6
" Pharmacokinetic analysis was performed using both non-compartmental and compartmental techniques."( Pharmacokinetics of florfenicol after a single intramuscular dose in white-spotted bamboo sharks (Chiloscyllium plagiosum).
Armstrong, DL; Cook, KK; Curro, TG; Dankoff, SM; Jaros, ND; Papich, MG; Vires, KW; Zimmerman, DM, 2006
)
0.33
" Pharmacokinetic parameters were calculated by a noncompartmental method."( Pharmacokinetics of florfenicol, thiamphenicol, and chloramphenicol in turkeys.
Debowy, J; Grabowski, T; Hrynyk, R; Jaworski, K; Okoniewski, P; Pawlowski, P; Smutkiewicz, A; Switała, M, 2007
)
0.62
"Clinical pharmacokinetic profiles were investigated following intramuscular (i."( Comparative pharmacokinetics of tylosin or florfenicol after a single intramuscular administration at two different doses of tylosin-florfenicol combination in pigs.
Chang, ZQ; Choi, JY; Gebru, E; Hwang, MH; Kang, EH; Kim, MH; Lim, JH; Park, SC; Yun, HI, 2008
)
0.35
" The method is suitable for the determination of low bergenin concentration in human plasma after therapeutic oral doses, and has been first and successfully used for its pharmacokinetic studies in healthy Chinese volunteers."( Determination of bergenin in human plasma after oral administration by HPLC-MS/MS method and its pharmacokinetic study.
Guo, RC; Liu, H; Wang, BJ; Wang, J; Wei, CM; Yuan, GY; Zhang, R; Zhang, XM, 2009
)
0.35
"The pharmacokinetic disposition and bioavailability of florfenicol (FF) were determined after single intravenous (i."( Pharmacokinetics of florfenicol after intravenous and intramuscular administration in New Zealand White rabbits.
Dogan, E; Kadioglu, Y; Koc, F; Okumus, Z; Ozturk, M; Yanmaz, LE, 2009
)
0.35
" The elimination half-life (t(1/2)(beta)), mean residence time (MRT), total body clearance (Cl(B)), area under the plasma concentration curve (AUC(0-infinity)) were different in chickens, pigeons and quail."( Comparative pharmacokinetics of florfenicol in the chicken, pigeon and quail.
El-Kattan, YA; Ismail, M, 2009
)
0.35
" Further pharmacodynamic studies in quail are needed to evaluate a suitable dosage regimen."( Pharmacokinetics of florfenicol in the plasma of Japanese quail.
Atila, A; Kadioglu, Y; Koc, F; Ozturk, M; Uney, K, 2009
)
0.35
" Significant differences in C(max) were detected between the plasma and muscle microdialysates, and between the breast and leg microdialysates of the Leghorn chickens by noncompartmental pharmacokinetic analysis."( Pharmacokinetics and tissue depletion of florfenicol in Leghorn and Taiwan Native chickens.
Chang, SK; Cheng, CN; Chou, CC; Davis, JL; Hsieh, MK; Koh, BW; Shien, RH, 2010
)
0.36
"A pharmacokinetic study of a commercial florfenicol-tylosin (2:1) combination product was conducted in six beagle dogs after intravenous (IV) and intramuscular (IM) administration at doses of 10 mg/kg (florfenicol) and 5 mg/kg (tylosin)."( Pharmacokinetics of a florfenicol-tylosin combination after intravenous and intramuscular administration to beagle dogs.
Gebru, E; Kim, EY; Kim, JC; Lee, JS; Park, SC, 2011
)
0.37
" Two-compartment model was selected to describe the pharmacokinetic characteristics of TG and TAP in vivo."( Pharmacokinetics of the prodrug thiamphenicol glycinate and its active parent compound thiamphenicol in beagle dogs following intravenous administration.
Chen, X; He, J; Lu, Y; Song, P; Yang, B; Zhao, D; Zheng, J; Zhu, J, 2011
)
0.65
" The elimination half-lives (t1/2β ), peak concentration of FF (Cmax ), and time to reach FF peak concentration (Tmax ) in plasma were estimated as 18."( Pharmacokinetics of florfenicol and its metabolite, florfenicol amine, in rice field eel (Monopterus albus) after a single-dose intramuscular or oral administration.
Chen, XX; Li, Q; Liu, H; Wu, ZX; Xie, LL; Yang, Y; Yuan, J, 2013
)
0.39
"This study evaluated the pharmacokinetic disposition of thiamphenicol (THA) and florfenicol (FLR) after oral administration of each at a single dose of 10 mg/kg body weight in Pacific white shrimp Litopenaeus vannamei held in freshwater at 25."( Pharmacokinetics and tissue distribution of thiamphenicol and florfenicol in Pacific white shrimp Litopenaeus vannamei in freshwater following oral administration.
Fang, W; Hu, L; Li, G; Li, X; Zhou, J; Zhou, S, 2013
)
0.9
" Serum concentrations were determined using a HPLC-UV assay and pharmacokinetic analysis was conducted using non-compartmental analysis."( Pharmacokinetics of florfenicol after intravenous and intramuscular dosing in llamas.
Lakritz, J; Niehaus, AJ; Pentecost, RL; Werle, NA, 2013
)
0.39
"4 for Cmax /MIC, 183 and 152 h for AUC0-24 h /MIC and 78 and 76 h for T>MIC."( Pharmacokinetic-pharmacodynamic integration and modelling of florfenicol in calves.
Illambas, J; Lees, P; Pelligand, L; Potter, T; Rassouli, A; Rycroft, A; Sidhu, P, 2014
)
0.4
") infusion of TG hydrochloride in healthy Chinese by evaluating the pharmacokinetic parameters, to provide clinical guidance in TG application."( Pharmacokinetics of thiamphenicol glycinate and its active metabolite by single and multiple intravenous infusions in healthy Chinese volunteers.
Chen, X; Li, N; Lu, Y; Qiu, Z; Song, P; Yang, B; Zhao, D, 2014
)
0.73
" The method herein described was superior to previous methods and was successfully applied to the pharmacokinetic study of TAP in healthy Chinese volunteers after oral administration."( UPLC-MS/MS determination of thiamphenicol in human plasma and its application to a pharmacokinetic study.
Cui, X; Huang, CK; Lian, QQ; Qiu, XJ; Sun, W; Wang, Z; Wang, ZS; Yang, H, 2014
)
0.7
"Experiments in different animal species have shown that febrile conditions, induced by Escherichia coli lipopolysaccharide (LPS), may alter the pharmacokinetic properties of drugs."( Pharmacokinetics of florfenicol after intravenous administration in Escherichia coli lipopolysaccharide-induced endotoxaemic sheep.
Drápela, C; Espinoza, A; Palma, C; Peñailillo, AK; Pérez, R; Sepulveda, M, 2015
)
0.42
" In the present study, we aimed to evaluate the effect of three coccidiostats, sulfaquinoxaline (SUL), robenidine (ROB), and toltrazuril (TOL), as feed additives on the pharmacokinetic profile of FFC in rabbits."( Influence of three coccidiostats on the pharmacokinetics of florfenicol in rabbits.
Liu, C; Shao, YX; Wang, SJ; Zhang, Q, 2015
)
0.42
"01) between FFC in situ forming gel and conventional injection, in pharmacokinetic parameters MRT (mean retention time) (57."( Study of pharmacokinetics of an in situ forming gel system for controlled delivery of florfenicol in pigs.
Geng, ZX; Li, HM; Liu, TF; Tian, J; Yu, ZG, 2015
)
0.42
" In synovial fluid, florfenicol pharmacokinetic parameters estimates were: mean Tmax 7 +/- 2 hours, mean t½ 64."( Synovial fluid pharmacokinetics of tulathromycin, gamithromycin and florfenicol after a single subcutaneous dose in cattle.
Coetzee, JF; Fajt, VR; Jones, ML; Rice, S; Washburn, KE, 2015
)
0.42
" A noncompartmental pharmacokinetic model was used for data analysis, and data were compared using the paired Student t-test."( The acute phase response induced by Escherichia coli lipopolysaccharide modifies the pharmacokinetics and metabolism of florfenicol in rabbits.
Burgos, R; Espinoza, A; Jeldres, JA; Palma, C; Peñailillo, AK; Pérez, R, 2016
)
0.43
" The maximum concentrations (Cmax , μg g(-1) or μg mL(-1) ) in plasma and tissues were observed at 2-6 h (the time to reach maximum concentration, Tmax ) except for bile (Tmax  = 24 h) and were in the order of intestine (52."( Pharmacokinetics of florfenicol and behaviour of its metabolite florfenicol amine in orange-spotted grouper (Epinephelus coioides) after oral administration.
Dong, JD; Feng, JB; Huang, DR; Liu, P; Zhong, M, 2016
)
0.43
" Pharmacokinetic data were pooled for two bioequivalent products, pioneer and generic formulations, administered intramuscularly to pigs at a dose rate of 15 mg/kg."( Pharmacokinetic/pharmacodynamic integration and modelling of florfenicol for the pig pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida.
Cheng, Z; Dorey, L; Lees, P; Pelligand, L, 2017
)
0.46
" In this study, a diffusion-limited physiologically based pharmacokinetic (PBPK) model was developed to predict the pulmonary pharmacokinetics of florfenicol (FF) in pigs."( Diffusion-limited PBPK model for predicting pulmonary pharmacokinetics of florfenicol in pig.
Gao, JD; Huang, LL; Ke, XB; Qian, MR; Sun, GZ; Wang, QY; Yang, B; Yang, H; Yang, JJ, 2017
)
0.46
" Pharmacokinetic parameters were estimated by noncompartmental methods and compared between the 2 formulations at each dose and route of administration."( Comparative pharmacokinetics of two florfenicol formulations following intramuscular and subcutaneous administration to sheep.
Angelos, JA; Balcomb, CC; Byrne, BA; Chigerwe, M; Holler, L; Lane, VM; Sahin, O; Tell, LA; Wetzlich, SE; Zhang, S, 2018
)
0.48
" The aim of this study was to evaluate the pharmacokinetic behavior of FF in turkeys in plasma, lung tissue, and pulmonary epithelial lining fluid (PELF)."( Pharmacokinetics of florfenicol in turkey plasma, lung tissue, and pulmonary epithelial lining fluid after single oral bolus or continuous administration in the drinking water.
Croubels, S; De Backer, P; De Baere, S; Devreese, M; Watteyn, A, 2018
)
0.48
" Pharmacokinetic parameters were calculated using a noncompartmental method."( Pharmacokinetics of florfenicol and thiamphenicol in ducks.
Poźniak, B; Smutkiewicz, A; Świtała, M; Tikhomirov, M, 2019
)
0.79
" In vitro transport assays using MDCK-chAbcg2 cells were conducted to assess chicken BCRP-mediated transport of FFC, while in vivo pharmacokinetic experiments with single or combined BCRP inhibitor gefitinib were employed to study the role of BCRP in oral FFC disposition."( Relevance of Breast Cancer Resistance Protein to Pharmacokinetics of Florfenicol in Chickens: A Perspective from In Vivo and In Vitro Studies.
Guo, L; Huang, J; Liu, Y; Wang, L; Zhang, Y; Zloh, M, 2018
)
0.48
" This study aimed to develop a population physiologically based pharmacokinetic (PBPK) model to predict the concentrations of FF and its metabolite, florfenicol amine (FFA), in cattle after four different routes of administration, and to calculate and compare the withdrawal intervals (WDIs) with approved withdrawal times based on different marker residues and their MRLs or tolerances."( Development and application of a population physiologically based pharmacokinetic model for florfenicol and its metabolite florfenicol amine in cattle.
Baynes, RE; Lin, Z; Riviere, JE; Yang, F, 2019
)
0.51
" Pharmacokinetic information regarding bath treatment is considerably lacking in comparison to other common administration routes."( Bath immersion pharmacokinetics of florfenicol in Nile tilapia (Oreochromis niloticus).
Chang, CC; Chou, CC; Hsieh, CY; Kuo, YS; Rairat, T, 2020
)
0.56
" This study evaluated the pharmacokinetic profiles of florfenicol (FF) and thiamphenicol (TP), which are synthetic bacteriostatic antimicrobial drugs, in geese after a single intravenous or oral administration, as well as seven oral doses administered at 12 h intervals."( Pharmacokinetics of florfenicol and thiamphenicol after single oral and intravenous, as well as multiple oral administrations to geese.
Poźniak, B; Smutkiewicz, A; Świtała, M; Tikhomirov, M, 2021
)
1.13
" Our study aims to develop the optimizing population physiologically-based pharmacokinetic (PBPK) model for assessing florfenicol residues in the tilapia tissues, and for evaluating the robustness of the withdrawal time (WT)."( Bayesian population physiologically-based pharmacokinetic model for robustness evaluation of withdrawal time in tilapia aquaculture administrated to florfenicol.
Chen, WY; Lin, HC, 2021
)
0.62
"Anaesthetics are commonly applied in pharmacokinetic (PK) studies to assure smooth handling of experimental procedures or to promote animal welfare."( Differential effects of aquatic anaesthetics on the pharmacokinetics of antibiotics: Examples using florfenicol in Nile tilapia (Oreochromis niloticus).
Chang, SK; Chi, Y; Chou, CC; Chuchird, N; Hsieh, CY; Rairat, T, 2021
)
0.62
" The elimination half-life was approx."( The influence of the site of drug administration on florfenicol pharmacokinetics in turkeys.
Bello, A; Poźniak, B; Smutkiewicz, A; Świtała, M, 2022
)
0.72
" Great efforts have been made to develop physiologically based pharmacokinetic (PBPK) models for estimating withdrawal intervals (WDIs) for extralabel prescribed drugs in food animals."( An Interactive Generic Physiologically Based Pharmacokinetic (igPBPK) Modeling Platform to Predict Drug Withdrawal Intervals in Cattle and Swine: A Case Study on Flunixin, Florfenicol, and Penicillin G.
Baynes, RE; Chou, WC; Davis, JL; Lin, Z; Maunsell, FP; Riviere, JE; Tell, LA, 2022
)
0.72
" Pretreatment with allicin changed the pharmacokinetic behavior of orally administered sulfadiazine, by increasing AUC (41."( Allicin affects the pharmacokinetics of sulfadiazine and florfenicol by downregulating the expression of jejunum P-gp and BCRP in broilers.
Fang, C; Gong, Q; Huang, J; Wang, L; Wang, X; Wang, Y; Zhang, Y, 2022
)
0.72
"Starvation has influence on physiology and pharmacokinetic (PK) characteristics of many drugs in land animals."( Effects of starvation on the pharmacokinetics and optimal dosages of florfenicol and associated serum biochemistry in Asian seabass (Lates calcarifer).
Chou, CC; Ho, WC; Hsieh, MK; Lu, YP; Rairat, T; Wu, HC, 2023
)
0.91
" Pharmacokinetic parameters were calculated using non-compartmental analysis."( Pharmacokinetics, tissue residue depletion, and withdrawal interval estimations of florfenicol in goats following repeated subcutaneous administrations.
Chen, Q; Clapham, MO; Davis, JL; Lin, Z; Tell, LA; Toney, E; Wetzlich, SE; Wu, X, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"The purpose of the present clinical studies was to determine the clinical efficacy of a combined parenteral and oral treatment with Bisolvon in combination with antibiotics in bovines suffering from acute respiratory disease."( [Treatment of acute respiratory tract diseases in cattle with Bisolvon in combination with either enrofloxacin, cefquinome, ceftiofur or florfenicol].
Hamel, U; Philipp, H; Quirke, JF; Schmidt, H, 1998
)
0.3

Bioavailability

ExcerptReferenceRelevance
" The intravenous route was chosen as reference and allowed the absolute bioavailability to be estimated."( Ocular pharmacokinetics of thiamphenicol in rabbits.
Aldana, I; Bruseghini, L; Ceppi Monti, N; Esteras, A; Figini, PG; Fos, D; Gazzaniga, A; Gianesello, V; Gonzalez Peñas, E; Zato, MA, 1992
)
0.58
" The bioavailability after intramuscular administration approached 100%."( The pharmacokinetics of thiamphenicol in lactating cows.
Alt, M; Errecalde, JO; Landoni, MF; Mestorino, N, 1993
)
0.59
" It was found that the drug is almost completely absorbed following intramuscular injection, with a bioavailability of about 87."( Thiamphenicol pharmacokinetics in sheep.
Abdennebi, EH; Khales, N; Sawchuk, RJ; Stowe, CM, 1994
)
1.73
" The bioavailability of florfenicol was 54% and 38% after intramammary and intramuscular administration, respectively."( Florfenicol pharmacokinetics in lactating cows after intravenous, intramuscular and intramammary administration.
Filep, R; Paape, MJ; Soback, S; Varma, KJ, 1995
)
0.29
" and oral route (30 mg/kg body weight) to study its plasma concentrations, kinetic behaviour, systemic bioavailability and tissue levels."( Tissue concentrations and pharmacokinetics of florfenicol in broiler chickens.
Afifi, NA; EL-SOOUD, KA, 1997
)
0.3
") and oral routes to study its plasma concentrations, kinetic behaviour, systemic bioavailability and tissue content."( Tissue concentrations and pharmacokinetics of florfenicol in broiler chickens.
Abo el-Sooud, KA; Afifi, NA, 1997
)
0.3
"6 hours) was longer than that after IV administration probably because of the slow absorption rate from the muscle."( Pharmacokinetics of thiamphenicol in dogs.
Arboix, M; Castells, G; Cristòfol, C; Franquelo, C; Intorre, L; Martí, G; Pérez, B, 1998
)
0.62
" administration, probably due to the slow rate of absorption from the muscle."( Thiamphenicol disposition in pigs.
Arboix, M; Castells, G; Cristòfol, C; El Korchi, G; Martì, G; Pérez, B; Prats, C, 1999
)
1.75
" The bioavailability of the drug was similar for the oral and intramuscular doses."( Pharmacokinetics of florfenicol after treatment of pigs with single oral or intramuscular doses or with medicated feed for three days.
D'Haese, E; De Craene, BA; De Riemaecker, D; Deprez, P; Nelis, H; Remon, JP; Vervaet, C; Voorspoels, J, 1999
)
0.3
" The extent of the protein binding and systemic bioavailability of florfenicol were 22."( Pharmacokinetic properties of florfenicol in Egyptian goats.
Abd El-Aty, AM; Atef, M; Aziza, MM; el-Gendi, AY, 2000
)
0.31
" Bioavailability was 101."( Pharmacodisposition of thiamphenicol in rabbits.
Abd El-Aty, AM; Abo El Sooud, K; Goudah, AM, 2001
)
0.62
", the bioavailability was about 60% in both species."( A comparative kinetic study of thiamphenicol in pre-ruminant lambs and calves.
Bertini, S; Giorgi, M; Intorre, L; Mengozzi, G; Secchiari, PL; Soldani, G, 2002
)
0.6
" administration, the bioavailability was estimated to be 91%, the peak plasma concentrations (Cmax) to be 10."( Pharmacokinetics of florfenicol in cod Gadus morhua and in vitro antibacterial activity against Vibrio anguillarum.
Bergh, O; Ervik, A; Samuelsen, OB, 2003
)
0.32
"The bioavailability and pharmacokinetic disposition of florfenicol in broiler chickens were investigated after intravenous (i."( Bioavailability and pharmacokinetics of florfenicol in broiler chickens.
Coats, JR; Hu, D; Shen, J; Wu, X, 2003
)
0.32
"A study on bioavailability and pharmacokinetics of florfenicol was conducted in 20 crossbred healthy sheep following a single intravenous (i."( Bioavailability and pharmacokinetics of florfenicol in healthy sheep.
Haiyang, J; Hsu, WH; Jiang, H; Jianzhong, S; Li, X; Shen, J; Walter, HH; Xiubo, L, 2004
)
0.32
"This study examined the disposition kinetics and bioavailability of florfenicol after intravenous (i."( Pharmacokinetics and bioavailability of florfenicol following intravenous, intramuscular and oral administrations in rabbits.
Abd El-Aty, AM; Abo El-Sooud, K; El-Zorba, HY; Goudah, A; Shimoda, M; Zhou, HH, 2004
)
0.32
" administration of florfenicol, the t(1/2), C(max), t(max) and oral bioavailability (F) were 15."( Pharmacokinetics of florfenicol and its metabolite, florfenicol amine, in the Korean catfish (Silurus asotus).
Kim, MS; Lim, JH; Park, BK; Yun, HI, 2006
)
0.33
" Differences in the bioavailability values of the compared fenicol antibiotics correspond to the ratio of the apolar/polar surface areas of their particles."( Pharmacokinetics of florfenicol, thiamphenicol, and chloramphenicol in turkeys.
Debowy, J; Grabowski, T; Hrynyk, R; Jaworski, K; Okoniewski, P; Pawlowski, P; Smutkiewicz, A; Switała, M, 2007
)
0.62
"A study on the bioavailability and pharmacokinetics of florfenicol was conducted in six healthy dogs following a single intravenous (i."( Pharmacokinetics of florfenicol and its metabolite, florfenicol amine, in dogs.
Hwang, YH; Kim, MS; Lim, JH; Park, BK; Yun, HI, 2008
)
0.35
" Together with highly variable bioavailability and erratic drinking-water uptake, these parameters resulted in the inability to reach a steady-state concentration through the continuous administration of florfenicol in the drinking water."( Induction of the carrier state in pigeons infected with Salmonella enterica subspecies enterica serovar typhimurium PT99 by treatment with florfenicol: a matter of pharmacokinetics.
Baert, K; Bousquet-Melou, A; de Backer, P; De Boever, S; Eeckhaut, V; Haesebrouck, F; Lanckriet, R; Martel, A; Pasmans, F; Van Immerseel, F, 2008
)
0.35
" Oral bioavailability was found to be 87 +/- 16%."( Plasma and tissue depletion of florfenicol and florfenicol-amine in chickens.
Anadón, A; Ares, I; Caballero, V; Martínez, M; Martínez, MA; Martínez-Larrañaga, MR; Ríos, A, 2008
)
0.35
"The pharmacokinetic disposition and bioavailability of florfenicol (FF) were determined after single intravenous (i."( Pharmacokinetics of florfenicol after intravenous and intramuscular administration in New Zealand White rabbits.
Dogan, E; Kadioglu, Y; Koc, F; Okumus, Z; Ozturk, M; Yanmaz, LE, 2009
)
0.35
" Mean absorption time (MAT), time to maximum concentration (T(max)), absorption half-life (t((1/2)ab)) and systemic bioavailability (F) were similar in the three species."( Comparative pharmacokinetics of florfenicol in the chicken, pigeon and quail.
El-Kattan, YA; Ismail, M, 2009
)
0.35
"To determine the pharmacokinetics and bioavailability of florfenicol in the plasma of healthy Japanese quail (Coturnix japonica)."( Pharmacokinetics of florfenicol in the plasma of Japanese quail.
Atila, A; Kadioglu, Y; Koc, F; Ozturk, M; Uney, K, 2009
)
0.35
" After I/M injection, the MRT, mean absorption time (MAT), and bioavailability were 12."( Pharmacokinetics of florfenicol in the plasma of Japanese quail.
Atila, A; Kadioglu, Y; Koc, F; Ozturk, M; Uney, K, 2009
)
0.35
" The absorption half-life (t(½ab)), C(max), AUMC, AUC and systemic bioavailability (F%) are significantly decreased, whereas elimination half-life (t(½el)) and MRT are increased in goats pre-treated by the three tested anthementics."( Effect of three anthelmentics on disposition kinetics of florfenicol in goats.
Abd El-Aty, AM; Amer, AM; Atef, M; El-Gendi, AY, 2010
)
0.36
" A rapid and nearly complete absorption of both drugs with a mean IM bioavailability of 103."( Pharmacokinetics of a florfenicol-tylosin combination after intravenous and intramuscular administration to beagle dogs.
Gebru, E; Kim, EY; Kim, JC; Lee, JS; Park, SC, 2011
)
0.37
"Nanotechnology applications in medicine have seen a tremendous growth in the past decade and are being employed to enhance the stability and bioavailability of lipophilic substances, such as florfenicol."( Nanoemulsion formulation of florfenicol improves bioavailability in pigs.
He, JK; Qian, MY; Tang, SS; Wei, L; Xiao, XL; Zhang, Q; Zhang, QJ; Zhang, ZJ; Zhou, D; Zhu, P, 2016
)
0.43
" The absorption rate constant and renal and hepatic clearance of FF were determined in vivo."( Diffusion-limited PBPK model for predicting pulmonary pharmacokinetics of florfenicol in pig.
Gao, JD; Huang, LL; Ke, XB; Qian, MR; Sun, GZ; Wang, QY; Yang, B; Yang, H; Yang, JJ, 2017
)
0.46
" Both antimicrobials showed rapid absorption and bioavailability of more than 70% indicating that PO route should be an efficient method of FF and TP administration to ducks under field conditions."( Pharmacokinetics of florfenicol and thiamphenicol in ducks.
Poźniak, B; Smutkiewicz, A; Świtała, M; Tikhomirov, M, 2019
)
0.79
" carinicauda, but elimination was slow and the bioavailability was not high."( Comparison of florfenicol pharmacokinetics in Exopalaemon carinicauda at different temperatures and administration routes.
Feng, Y; Li, J; Wang, J; Zhai, Q, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" In addition, the renal portal system in birds may reduce the bioavailability of the drug administered in the caudofemoral region of the body."( The influence of the site of drug administration on florfenicol pharmacokinetics in turkeys.
Bello, A; Poźniak, B; Smutkiewicz, A; Świtała, M, 2022
)
0.72

Dosage Studied

Thiamphenicol is present as glycinate hydrochloride (TG) and glycinate acetylcysteinate (TGA) esters in the parenteral and aerosol dosage form. Five rabbits were each given a single 30 mg/kg of body weight dosage by intravenous (i.e. IV) treatment.

ExcerptRelevanceReference
"Thiamphenicol at the rate of 50 mg/kg/day given to female NZBxOUW F1 hybrid mice from weaning and continuing throughout life resulted in a considerable extension of lifespan, although this was less than in mice given the same drug dosage from first antinuclear antibody (ANA) positivity (Simpson, Aarons and Howie, 1979)."( Thiamphenicol and lupus nephritis. II. The effects of giving the drug from weaning to NZBxOUW F1 hybrid female mice.
Aarons, I; Howie, JB; Simpson, LO, 1979
)
3.15
" Dose-response relationships differ depending on the date and duration of treatment."( Embryonic development and mitochondrial function. 2. Thiamphenicol induced embryotoxicity.
Bass, R; Oerter, D, 1977
)
0.51
" With the dosage applied, minimum concentrations required for the inhibition of many Gram-positive and Gram-negative organisms causing intrauterine infections were attained in maternal plasma, cord plasma and amniotic fluid."( Placental transfer of thiamphenicol in term pregnancy.
Maes, RA; Plomp, TA; Thiery, M, 1977
)
0.57
" With the dosage applied, minimum concentrations required for the inhibition of many organisms causing intrauterine infections were reached in maternal and fetal plasma and in amniotic fluid."( Placental transfer of thiamphenicol.
Maes, RA; Plomp, TA; Thiery, M; Yo Le Sian, A, 1976
)
0.57
" Thiamphenicol is well tolerated at this dosage and appears to be an excellent treatment for acute salpingitis."( Thiamphenicol for treatment of salpingitis.
Henrion, RM; Vige, PM,
)
2.48
" This condition can be avoided by reduction of dosage and by monitoring levels of drug in the serum of these infants."( Chloramphenicol: A review of its use in clinical practice.
Feder, HM; Maderazo, EG; Osier, C,
)
0.13
" 4) Drug concentrations (greater than 3--5 micrograms/g wet weight) obtained with dosing regimens (greater than 100 mg/kg/day) used for experimental induction of embryolethality in rats are equal to those necessary for inhibition of mitochondrial protein synthesis in vitro and to those necessary for treatment of bacterial infections in man."( Placental transfer of thiamphenicol in the rat.
Bass, R; Nau, H, 1981
)
0.58
"IN a crossover design study, 3 dogs were given TAP IV, and 3 dogs were given TAP IM, each at a dosage of 40 mg/kg of body weight."( Pharmacokinetics of thiamphenicol in dogs.
Arboix, M; Castells, G; Cristòfol, C; Franquelo, C; Intorre, L; Martí, G; Pérez, B, 1998
)
0.62
" Five rabbits were each given thiamphenicol as a single 30 mg/kg of body weight dosage by intravenous (i."( Pharmacodisposition of thiamphenicol in rabbits.
Abd El-Aty, AM; Abo El Sooud, K; Goudah, AM, 2001
)
0.91
"Approaches involved dosing mice with thiamphenicol (TAP) to yield staged cohorts of pro-erythroid cells; optimizing conditions for their EPO-dependent in vitro growth and survival; developing assays for CFU-E maturation; analyzing stage-specific transcript expression; and expressing a heterologous, erythroid-specific tag (EE372) in transgenic mice."( An optimized system for studies of EPO-dependent murine pro-erythroblast development.
Geiger, JN; Johnson, MM; Miller, CP; Pircher, TJ; Wojchowski, DM; Zhang, D, 2001
)
0.58
" Thiamphenicol is present as glycinate hydrochloride (TG) and glycinate acetylcysteinate (TGA) esters in the parenteral and aerosol dosage form."( Recent clinical evidence of the efficacy and safety of thiamphenicol glycinate acetylcysteinate and thiamphenicol glycinate.
De Benedetto, F; Grassi, C, 2002
)
1.47
" Female BALB/c mice were gavaged with TAP, daily for 7-17 days at 400-1500 mg/kg; female Wistar Hanover rats were dosed with TAP daily at 50-375 mg/kg for 9 or 10 days."( Haemotoxicity of thiamphenicol in the BALB/c mouse and Wistar Hanover rat.
Andrews, CM; Gibson, FM; Havard, AC; Robinson, S; Turton, JA; Williams, TC; York, M, 2002
)
0.65
" When a drug product is dosed via drinking water in a farm setting, a number of variables, including pH, chlorine content, hardness of the water used for dilution, and container material, may affect its stability, leading to a decrease in drug potency."( Stability of florfenicol in drinking water.
Eichman, J; Gilewicz, R; Hayes, JM; Katz, T,
)
0.13
" Florfenicol was developed as an injectable antibiotic for use in cattle on an every other day dosing schedule."( Use of florfenicol in non-human primates.
Cook, AL; Sams, R; St Claire, M, 2004
)
0.32
" Five dosage levels of FFC in medicated feed were administered daily: 0, 5, 10, 15, and 30 mg of active ingredient/kg of fish body weight."( Laboratory efficacy of florfenicol against Streptococcus iniae infection in sunshine bass.
Darwish, AM, 2007
)
0.34
" Patients were randomized to treatment with thiamphenicol glycinate acetylcysteinate, dosage 250 mg/day in 2 administrations plus beclomethasone with a dosage of 400 microg/day in 2 administrations, or no treatment, control group, unless required."( Aerosol antibiotic therapy in children with chronic upper airway infections: a potential alternative to surgery.
Castelnuovo, P; Macchi, A,
)
0.39
" Further pharmacodynamic studies in quail are needed to evaluate a suitable dosage regimen."( Pharmacokinetics of florfenicol in the plasma of Japanese quail.
Atila, A; Kadioglu, Y; Koc, F; Ozturk, M; Uney, K, 2009
)
0.35
"A dose titration study was conducted to determine the dosage of florfenicol (FFC) in feed to control Streptococcus iniae-associated mortality in Nile tilapia Oreochromis niloticus."( Determination of florfenicol dose rate in feed for control of mortality in Nile tilapia infected with Streptococcus iniae.
Baumgartner, W; Camus, A; Endris, R; Gaunt, PS; McGinnis, A; Steadman, J; Sun, F; Sweeney, D, 2010
)
0.36
" Results from these studies support that 10 mg florfenicol/kg body weight in channel catfish is an efficacious dosage following oral administration."( Single intravenous and oral dose pharmacokinetics of florfenicol in the channel catfish (Ictalurus punctatus).
Adams, P; Crouch, L; Endris, R; Gao, D; Gaunt, PS; Langston, C; Sweeney, D; Wrzesinski, C, 2012
)
0.38
" Dosing to achieve MPC concentrations (where possible) may serve to reduce the selection of bacterial subpopulations with reduced antimicrobial susceptibility."( Comparative minimum inhibitory and mutant prevention drug concentrations of enrofloxacin, ceftiofur, florfenicol, tilmicosin and tulathromycin against bovine clinical isolates of Mannheimia haemolytica.
Blondeau, BJ; Blondeau, JM; Blondeau, LD; Borsos, S; Hesje, CE, 2012
)
0.38
" Feed consumption was only affected during the last 10 dosing days when the 45 and 75 mg/kg groups consumed only 62."( Safety of florfenicol administered in feed to tilapia (Oreochromis sp.).
Endris, RG; Gaikowski, MP; Schleis, SM; Tuomari, D; Wolf, JC, 2013
)
0.39
" The aim of this study was to evaluate the depletion of florfenicol and its major metabolite, florfenicol amine, from the edible tissue of two fish species, rainbow trout and sea bream, following treatment with medicated feed at a dosage of 10 mg kg(-1) of bw day(-1) , for 10 consecutive days."( Florfenicol depletion in edible tissue of rainbow trout, Oncorhynchus mykiss (Walbaum), and sea bream, Sparus aurata L.
della Rocca, G; Di Salvo, A; Malvisi, J; Terzetti, E, 2013
)
0.39
" These data form a rational basis for dosage selection for treatment of calf pneumonia caused by M haemolytica or P multocida."( Pharmacodynamics of florfenicol for calf pneumonia pathogens.
Cheng, Z; Illambas, J; Lees, P; Potter, T; Rycroft, AN; Sidhu, P, 2013
)
0.39
" dosing was 3h."( Pharmacokinetics of florfenicol after intravenous and intramuscular dosing in llamas.
Lakritz, J; Niehaus, AJ; Pentecost, RL; Werle, NA, 2013
)
0.39
" More research into determination of PK/PD targets of efficacy is needed to further assess the clinical use of chloramphenicol and florfenicol as second-line agents in dogs, optimize dosage regimens, and set up species-specific clinical break points."( In vitro assessment of chloramphenicol and florfenicol as second-line antimicrobial agents in dogs.
Guardabassi, L; Maaland, MG; Mo, SS; Schwarz, S, 2015
)
0.42
" dosing was also prolonged (p = 0."( Absorption and disposition of florfenicol after intravenous, intramuscular and subcutaneous dosing in alpacas.
Lakritz, J; Niehaus, AJ; Pentecost, RL; Werle, N, 2015
)
0.42
" The results demonstrated that the in situ forming gel system could shorten dosing interval of FFC and thus achieved less frequent administration during long-term treatment."( Study of pharmacokinetics of an in situ forming gel system for controlled delivery of florfenicol in pigs.
Geng, ZX; Li, HM; Liu, TF; Tian, J; Yu, ZG, 2015
)
0.42
" Several product labels provided inadequate information on how to calculate therapeutic dosage and further stated withdrawal time despite lack of pharmacokinetic data on the antimicrobials in catfish."( Quality of Antimicrobial Products Used in Striped Catfish (Pangasianodon hypophthalmus) Aquaculture in Vietnam.
Dalsgaard, A; Phu, TM; Phuong, NT; Scippo, ML, 2015
)
0.42
" The effects of pH, pressure and Flo concentration on removal efficiency of NF and the effects of pH, Flo concentration and dosage of hydrogen peroxide and contact time on the AOP are assessed."( Treatment of florfenicol of synthetic trout fish farm wastewater through nanofiltration and photocatalyst oxidation.
Cheshmberah, F; Esmaili, Z; Farhadian, M; Solaimany Nazar, AR, 2017
)
0.46
" These data indicate the value of using a biological medium, when determining microbiological potency indices, to predict dosage for clinical use."( Activity of florfenicol for Actinobacillus pleuropneumoniae and Pasteurella multocida using standardised versus non-standardised methodology.
Dorey, L; Hobson, S; Lees, P, 2016
)
0.43
" We characterized the toxicokinetics of FLR in the swimming crab (Portunus trituberculatus) after intravenous (IV) dosing (20, 40 and 80mg/kg)."( Effects of florfenicol on the antioxidant status, detoxification system and biomolecule damage in the swimming crab (Portunus trituberculatus).
Gao, B; Li, J; Liu, P; Ren, X; Wang, Z, 2017
)
0.46
"Pharmacokinetic-pharmacodynamic (PK/PD) integration and modelling were used to predict dosage schedules for florfenicol for two pig pneumonia pathogens, Actinobacillus pleuropneumoniae and Pasteurella multocida."( Pharmacokinetic/pharmacodynamic integration and modelling of florfenicol for the pig pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida.
Cheng, Z; Dorey, L; Lees, P; Pelligand, L, 2017
)
0.46
" The model accurately predicted the concentration-time courses of FF in lung interstitial fluid, serum, and plasma following different dosing schedules, except at the dose of 15 mg/kg."( Diffusion-limited PBPK model for predicting pulmonary pharmacokinetics of florfenicol in pig.
Gao, JD; Huang, LL; Ke, XB; Qian, MR; Sun, GZ; Wang, QY; Yang, B; Yang, H; Yang, JJ, 2017
)
0.46
"For all organisms and all drugs investigated in this study, it is suggested that broth MICs should be adjusted by an appropriate scaling factor when used to determine pharmacokinetic/pharmacodynamic breakpoints for dosage prediction."( Impact of growth matrix on pharmacodynamics of antimicrobial drugs for pig pneumonia pathogens.
Dorey, L; Lees, P, 2017
)
0.46
" MPC concentrations provide a dosing target which may serve to reduce amplification of bacterial subpopulations with reduced antimicrobial susceptibility."( Mutant prevention and minimum inhibitory concentration drug values for enrofloxacin, ceftiofur, florfenicol, tilmicosin and tulathromycin tested against swine pathogens Actinobacillus pleuropneumoniae, Pasteurella multocida and Streptococcus suis.
Blondeau, JM; Fitch, SD, 2019
)
0.51
" The long-acting injectable preparation of doxycycline was well tolerated by koalas when administered via the subcutaneous route, and the weekly dosing requirement is a major advantage when treating wild animals."( Clinical comparison of five anti-chlamydial antibiotics in koalas (Phascolarctos cinereus).
Booth, R; Nyari, S, 2020
)
0.56
" Thus, the selected FF and TP dosage may be considered as a safe treatment for geese."( Pharmacokinetics of florfenicol and thiamphenicol after single oral and intravenous, as well as multiple oral administrations to geese.
Poźniak, B; Smutkiewicz, A; Świtała, M; Tikhomirov, M, 2021
)
0.9
" Fitting with published pharmacokinetic profiles that experimented under temperatures of 22 and 28 °C, a PBPK model was constructed by applying with the Bayesian Markov chain Monte Carol (MCMC) algorithm to estimate WTs under different physiological, environmental and dosing scenarios."( Bayesian population physiologically-based pharmacokinetic model for robustness evaluation of withdrawal time in tilapia aquaculture administrated to florfenicol.
Chen, WY; Lin, HC, 2021
)
0.62
" Whether or not the numbers and extent of PK parameters change mitigate subsequent estimations of other PK-derived secondary values such as dosing regimen and withdrawal time remains to be elucidated, but the auxiliary use of anaesthetics in PK studies should not assume uninfluential."( Differential effects of aquatic anaesthetics on the pharmacokinetics of antibiotics: Examples using florfenicol in Nile tilapia (Oreochromis niloticus).
Chang, SK; Chi, Y; Chou, CC; Chuchird, N; Hsieh, CY; Rairat, T, 2021
)
0.62
" This study assessed the safety of 30 days of oral florfenicol (FFC) dosing at 0-10 times the therapeutic dose (1 × : 10 mg/kg biomass/day) in Oreochromis niloticus juveniles."( The effects of extended feeding of florfenicol coated medicated diets on the safety, serum biomarkers and blood cells morphology of Nile tilapia Oreochromis niloticus (L.).
Abraham, TJ; Bardhan, A; Patil, PK; Saha, S; Sarker, S; Singha, J, 2022
)
0.72
" Overall, FF absorption, distribution, and elimination rates were reduced by starvation, resulting in four to five times lower optimal dosage than the non-starved fish."( Effects of starvation on the pharmacokinetics and optimal dosages of florfenicol and associated serum biochemistry in Asian seabass (Lates calcarifer).
Chou, CC; Ho, WC; Hsieh, MK; Lu, YP; Rairat, T; Wu, HC, 2023
)
0.91
"v bolus of florfenicol solution and dosed orally with FSRGs in the fasting and fed states."( Florfenicol sustained-release granules: an in vitro-in vivo correlation study in pigs.
Huang, XH; Liu, ZY; Shen, Y; Xu, Y; Yang, WC; Yu, Y; Zhang, YX, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
immunosuppressive agentAn agent that suppresses immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-cells or by inhibiting the activation of helper cells. In addition, an immunosuppressive agent is a role played by a compound which is exhibited by a capability to diminish the extent and/or voracity of an immune response.
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
sulfoneAn organosulfur compound having the structure RS(=O)2R (R =/= H).
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency3.57080.000811.382244.6684AID686978; AID686979
EWS/FLI fusion proteinHomo sapiens (human)Potency16.27840.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
retinoid X nuclear receptor alphaHomo sapiens (human)Potency23.91450.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency1.55590.001530.607315,848.9004AID1224849
estrogen nuclear receptor alphaHomo sapiens (human)Potency62.47540.000229.305416,493.5996AID743069
cytochrome P450 2D6Homo sapiens (human)Potency15.48710.00108.379861.1304AID1645840
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)2.37900.06008.9128130.5170AID1902; AID1914
Estrogen receptorRattus norvegicus (Norway rat)EC50 (µMol)4.01800.006022.3670130.5170AID1914
Estrogen receptor betaRattus norvegicus (Norway rat)EC50 (µMol)4.01800.006022.3670130.5170AID1914
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (103)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID29421Partition coefficient (logP) (HPLC)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID69585Tested for inhibition of puromycin reaction and reported as equilibrium constant derived from primary and secondary kinetic plots for the inhibition of peptide bond formation1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Aminoacyl analogs of chloramphenicol: examination of the kinetics of inhibition of peptide bond formation.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID27580Partition coefficient (logP)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID563230Antimicrobial activity against apramycin-resistant cmlR2 null mutant Streptomyces coelicolor B756 after 48 hrs relative to wild type2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Two distinct major facilitator superfamily drug efflux pumps mediate chloramphenicol resistance in Streptomyces coelicolor.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID19427HPLC capacity factor (k)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (944)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990253 (26.80)18.7374
1990's62 (6.57)18.2507
2000's167 (17.69)29.6817
2010's318 (33.69)24.3611
2020's144 (15.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 66.86

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index66.86 (24.57)
Research Supply Index7.04 (2.92)
Research Growth Index4.86 (4.65)
Search Engine Demand Index115.81 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (66.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials100 (9.57%)5.53%
Reviews24 (2.30%)6.00%
Case Studies36 (3.44%)4.05%
Observational0 (0.00%)0.25%
Other885 (84.69%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double Blind, Placebo Controlled, Parallel Group Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of 14-Day Repeated-Dose Administration of Thiamphenicol (RUX 122) in Healthy Subjects [NCT00958503]Phase 130 participants (Actual)Interventional2007-07-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]